75424-70-3Relevant articles and documents
Mild and Regioselective N-Alkylation of 2-Pyridones in Water
Hao, Xin,Xu, Zhongmiao,Lu, Hongfu,Dai, Xuedong,Yang, Ting,Lin, Xichen,Ren, Feng
supporting information, p. 3382 - 3385 (2015/07/28)
A mild and regioselective N-alkylation reaction of 2-pyridones in water has been developed. Tween 20 (2% w/w) was added to create a micellar system for improved solubility of starting materials, which leads to enhanced reaction rates. The protocol demonstrated a wide substrate scope with good isolated yields (40-94%) for all of the 24 examples evaluated. High regioselectivity favoring N-alkylation over O-alkylation was observed for benzyl halides (>5:1), primary alkyl halides (>6:1), and bulky and less reactive secondary alkyl halides (>2.4:1).
Pyrazole compounds and their use as antidiabetes agents
-
, (2008/06/13)
The present invention provides a pyrazole compound that has liver glycogen phosphorylase inhibitory activity and is useful as a therapeutic or prophylactic agent for diabetes, the pyrazole compound represented by the following general formula (I): wherein Ring Q represents an aryl or heteroaromatic group, R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azido group, R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group, an azido group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group, R4 and R5 are identical with or different from each other and represent a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, a C3-8 cycloalkyl group, a substituted or unsubstituted saturated heterocyclic group, a substituted or unsubstituted aryl group, a C7-14 aralkyl group, a heteroaromatic group, or the like, or a pharmacologically acceptable salt thereof.
PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME
-
Page/Page column 249-250, (2008/06/13)
A pyrazole compound represented by the general formula (I) or a salt thereof which has a hepatic glycogen phosphorylase inhibitory activity and therefore is useful as a therapeutic or prophylactic agent for diabetes or a pharmacologically salt thereof : wherein the ring Q represents an aryl group or an aromatic heterocyclic group; R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azide group; R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo-C1-6 alkyl group, a C1-6 alkoxy group, an azide group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group; R4 and R5 independently represent a hydrogen atom, a C1-6 alkyl group which may be substituted, a a C3-8 cycloalkyl group, a saturated heterocyclic group which may be substituted, an aryl group which may be substituted, a C7-14 aralkyl group, an aromatic heterocyclic group or the like.
Pyrimidine derivatives useful as inhibitors of PKC-theta
-
Page/Page column 119, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
